Cubebin and derivatives as inhibitors of mitochondrial complex I. Proposed interaction with subunit B8.
J Enzyme Inhib Med Chem
; 24(2): 599-606, 2009 Apr.
Article
em En
| MEDLINE
| ID: mdl-18825534
ABSTRACT
The effects on mitochondrial respiration and complex I NADH oxidase activity of cubebin and derivatives were evaluated. The compounds inhibited the state 3 glutamate/malate-supported respiration of hamster liver mitochondria with IC(50) values ranging from 12.16 to 83.96 microM. NADH oxidase reaction was evaluated in submitochondrial particles. The compounds also inhibited this activity, showing the same order of potency observed for effects on state 3 respiration, as well as a tendency towards a non-competitive type of inhibition (K(I) values ranging from 0.62 to 16.1 microM). A potential binding mode of these compounds with complex I subunit B8, assessed by docking calculations, is proposed.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Lignanas
/
Complexo I de Transporte de Elétrons
Limite:
Animals
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article